By: Isao Ueyama, Shin Kurogochi, Itsuroh Kobori, Toshiaki Hoshino, Yoichi Ishii, and Iwao Takase
Two deuterium labels of pencycuron [1-(p-chlorobenzyl)-1-cyclopentyl-3-phenylurea],pentadeuteriolabeled at the phenyl group and tetradeuteriolabeled at the 2,2,5,5 positions of the cyclopentyl group,were synthesized. Each was mixed with equimolar nonlabeled pencycuron and administered orally to male rabbits. Excreta were purified and subjected to GC-MS, and 11 metabolites(urine,11;feces,3) were characterized by ion cluster analysis. Major urinary metablites were 1-(p-chlorobenzyl)-1-cyclopencyl-3-(p-hydroxyphenyl)urea (free and glucruonide).Decyclopentylation,hydroxylation at the 3 position of the cyclopentyl moiety,diol formations,thiomethylation at the phenyl ring,and some other glucuronides were also observed in the metabolites. Three mass spectra of fully methylated glucuronides were obtained in intact form. Besides three minor metabolites, a significant amount of fecal pencycuron was found. A metabolic scheme is proposed to fit the adta obtained.
Two deuterium labels of pencycuron [1-(p-chlorobenzyl)-1-cyclopentyl-3-phenylurea],pentadeuteriolabeled at the phenyl group and tetradeuteriolabeled at the 2,2,5,5 positions of the cyclopentyl group,were synthesized. Each was mixed with equimolar nonlabeled pencycuron and administered orally to male rabbits. Excreta were purified and subjected to GC-MS, and 11 metabolites(urine,11;feces,3) were characterized by ion cluster analysis. Major urinary metablites were 1-(p-chlorobenzyl)-1-cyclopencyl-3-(p-hydroxyphenyl)urea (free and glucruonide).Decyclopentylation,hydroxylation at the 3 position of the cyclopentyl moiety,diol formations,thiomethylation at the phenyl ring,and some other glucuronides were also observed in the metabolites. Three mass spectra of fully methylated glucuronides were obtained in intact form. Besides three minor metabolites, a significant amount of fecal pencycuron was found. A metabolic scheme is proposed to fit the adta obtained.
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